title: Benzylidene 2-aminoimidazolones derivatives: synthesis and in vitro evaluation of anti-tumor carcinoma activity.
abstract: A series of benzylidene 2-aminoimidazolones derivatives were synthesized. Most compounds displayed strong inhibitory activity on the proliferation of human HepG2 cells in vitro. The active compounds were further evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against five human cancer cell lines in vitro. Compound 2b exhibited the strongest antitumor activities with IC₅₀ values ranging from 12.87-17.10 µM which were nearly 1-3.5 fold less than that of 5-FU (IC₅₀=18.39-56.12 µM) in vitro. Furthermore, compound 2b could induce SMMC-7721 cell apoptosis in a dose-dependent manner. Therefore, our novel findings may provide a new framework for the design of new benzylidene 2-aminoimidazolones derivatives for the treatment of cancer.
authors.affiliation: Medical College, Nantong University.
authors.forename: Yong
authors.initials: Y
authors.lastname: Ling
authors.forename: Zhi-Qiang
authors.initials: ZQ
authors.lastname: Wang
authors.forename: You-An
authors.initials: YA
authors.lastname: Xiao
authors.forename: Chenyu
authors.initials: C
authors.lastname: Zhu
authors.forename: Liucen
authors.initials: L
authors.lastname: Shen
authors.forename: Xue-Min
authors.initials: XM
authors.lastname: Wang
authors.forename: Yi
authors.initials: Y
authors.lastname: Hui
authors.forename: Xin-Yang
authors.initials: XY
authors.lastname: Wang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D001597:Benzylidene Compounds / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001597:Benzylidene Compounds; D007093:Imidazoles; C117197:imidazolone